Endorphines are essentially protein hormones produced in the hypothalamic brain region, the site of synthesis of said substances being encephalic subcortical nuclei. Endorphines act as neuromediators and perform numerous most diverse functions in organism, the most important of such a variety thereof being a regulatory function of pain sense modality. Being neiromediators, endorphines have an effect on emotional responses by causing one to feel pleasure. Compounds of said class regulate state of hunger, are engaged in memory processes, in organism's response to stress-factors, in emotional disorders and reactions to alcohol, they normalize arterial tension, respiration rate, renal activity, and functioning of the digestive system. It is found experimentally that endorphines promote healing of injured tissues, callus formation in fractures and add to general resistance to sepsis.
In all chronic diseases, secondary effects of stress or depression, declining creative activity there is observed deficiency of endorphines, the causes of which may be most diverse, that is, pathologies of endocrine system, genetic features of organism, infection factor (some viruses inhibit hormonopoiesis of pleasure hormones), dejected mood, perpetual dissatisfaction with oneself and with one's associates.
Normal synthesis of endorphines is deranged also as a result of presence of opiates, e.g., heroin (diacetylmorphine) in organism. Once the opiate introduced into the organism has been destroyed, the level of endorphines therein remains abnormally low, because an euphoria-causative effect of said opiates is due to their being attached to cerebral receptors for endorphines. Abnormally low brain level of endorphines causes physical and emotional pain. To release oneself from pain, the sufferer is compelled to take a great dose of a narcotic, whereby a chemical dependence on opiates is being developed. It is at least a few days should pass until the brain resumes generating endorphines.
One of the methods to increase producing of endorphines is acupuncture which conduces to releasing the available endorphines. Devices that relieve heavy pain by applying a weak electric signal to skin, stimulate generating endorphines. Running or other physical exercises are also causative of increasing release of endorphines under such loads. That is why just regular physical exercises are given such importance in prevention and rehabilitation programs of control of chemical dependence on opiates.
However, said methods are but inadequately effective for therapy of pathologic conditions concerned with deficiency of endorphines in organism.
Known in the present state of the art is a method for increasing the level β-endorphine contained in hypothalamus and hypophysis (cf. “Effect of EMP at the level of β-endorphines in the brain” by V. F. Pavlovski, V. F. Katkov, S. E. Dyakov, said method being a non-pharmacological method of acting upon principal neurochemical mechanisms of CNS functioning forming the basis of nociperception processes, forming an emotional status, stress response, education and memory, drug dependence syndrome and drug addiction.
All endorphines are polypeptides, β-endorphine being a fragment of β-lipotropin, another polypeptide also detectable in hypothalamus and hypophysis. The method consists in that test animals (120 albino rat males each weighing 180-200 g) are exposed to irradiation with a low-energy (specific irradiation energy up to 10 μW/sq.cm) with a pulse-modulated microwave field having characteristics obtained by mathematical simulation on the basis of applying the theory of non-linear pendulums and resonance phenomena to control over biological processes. Upon completing the experiments the test animals are decapitated and the hypothalamus is immediately isolated, the tissue is weighed and rapidly subjected to homogenization with a tenfold volume of 0.2 N HCl solution heated to 95° C. over a boiling water bath. In 15 minutes the tissue specimens are cooled in an ice bath before homogenization and further procedures and β-endorphine is extracted for a two-hour period at t=4° C. and is subjected to centrifuging in a cryocentrifuge at 4500 rpm for 20 minutes. Then the translucent post-centrifugal supernatant fluid is decanted into preprepared test tubes. Then the β-endorphine-containing extracts are frozen and lyophilized by freeze drying. Thereupon the β-endorphine content of the cerebral tissues in the test animals is identified by a high-sensitivity radio-immunoassay method. The fundamental of the method is based on high antiserum sensitivity to β-endorphine. Immediately before the radioassay the specimens are dissolved in a p.1 M borate buffer with pH=8.4 containing 1% bovine albumin. All opiopeptide determination procedures are conducted over an ice bath at t=0 to +2° C. Exposure to the effect of modulated microwave fields leads to a substantial change in the β-endorphine level.
However, the known method is extremely sophisticated technologically and therefore is of little use in therapeutic practice.
A variety of synthetic endorphine analogs were provided having selective effect on one receptors or other. Known in the present state of the art is a powder-like biogenic preparation from ossified deer antlers (cf. RU, A, 2,077,887) which comprises a complex of biologically potent components—amino acids, peptides, lipids, carbohydrates, steroid hormones, fatty acids, organophosphorous compound, as well as a great amount of micro- and macroelements (potassium, calcium, iron, magnesium, zinc, copper, manganine, nickel, tin, chromium, lithium, baryum, and others). It is due a unique composition of the powder ingredients that there is attainable multimodality of treatment effect produced on human organism so as to provide increase in adaptogenic resources which normalizes metabolic effect comprising correction of lipid, protein and carbohydrate metabolism, regulation of redox and hemopoietic processes, increasing immunobiological and body defenses, stimulation of growth and development of osseomuscular tissue, excretion of heavy metals and toxins from organism, and the like.
The present biogenic preparation with preserved natural-origin activity of the starting product has a broad range of pharmacological action which is not yet studied thoroughly. This in turn prevents its use as a drug for therapy of metabolic disorders and hormonal dysfunction, as well as in narcological practice.